BR0307720A - Alkali Metal Addition Stabilized Atorvastatin Formulations, Method for Producing a Pharmaceutical Formulation and Stabilizing Said Formulation - Google Patents

Alkali Metal Addition Stabilized Atorvastatin Formulations, Method for Producing a Pharmaceutical Formulation and Stabilizing Said Formulation

Info

Publication number
BR0307720A
BR0307720A BR0307720-9A BR0307720A BR0307720A BR 0307720 A BR0307720 A BR 0307720A BR 0307720 A BR0307720 A BR 0307720A BR 0307720 A BR0307720 A BR 0307720A
Authority
BR
Brazil
Prior art keywords
atorvastatin
sodium
magnesium
formulation
alkali metal
Prior art date
Application number
BR0307720-9A
Other languages
Portuguese (pt)
Inventor
Bharat Romi Singh
Manoj Pananchukunnath Kumar
Rajiv Malik
Original Assignee
Ranbaxi Lab Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ranbaxi Lab Ltd filed Critical Ranbaxi Lab Ltd
Publication of BR0307720A publication Critical patent/BR0307720A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles

Abstract

"FORMAçõES DE ATORVASTATINA ESTABILIZADAS COM ADIçõES DE METAL ALCALINO, MéTODO PARA PRODUZIR UMA FORMULAçãO FARMACêUTICA E ESTABILIZAR DITA FORMULAçãO". A presente invenção refere-se a uma formulação farmacêutica tendo melhorada biodisponibilidade e bioequivalência que inclui partículas de atorvastatina amorfa e/ou cristalina que têm um tamanho de partícula (d~ 90~) menor que 150 <109>m e um tamanho médio de partícula (d~ 50~) que fica entre aproximadamente 5 e 50 <109>m. A atorvastatina pode ser uma ou mais entre atorvastatina cálcio, atorvastatina magnésio, atorvastatina alumínio, atorvastatina ferro e atorvastatina zinco. As formulações de atorvastatina podem ser estabilizadas pela mistura de atorvastatina com um aditivo de sal de metal alcalino a uma concentração entre aproximadamente 1,2% e menos que 5% peso/peso da formulação. O aditivo de sal de metal alcalino pode ser um ou mais entre carbonato de sódio, bicarbonato de sódio, hidróxido de sódio, silicato de sódio, ortofosfato mono-hidrogênio dissódico, fosfato di-hidrogênio de sódio, fosfato mono-hidrogênio dissódico, fosfato de sódio, aluminato de sódio, carbonato de cálcio, hidróxido de cálcio, carbonato de magnésio, hidróxido de magnésio, silicato de magnésio, aluminato de magnésio e hidróxido de alumínio e magnésio. As formulações de atorvastatina podem ser usadas para tratar condições médicas, incluindo hipercolesterolemia primária, disbetalipoproteinemia e hipercolesterolemia homozigótica familiar."ATORVASTATIN FORMATIONS STABILIZED WITH ALKALINE METAL ADDITIONS, METHOD FOR PRODUCTING PHARMACEUTICAL FORMULATION AND STABILIZING DITA FORMULATION". The present invention relates to a pharmaceutical formulation having improved bioavailability and bioequivalence that includes amorphous and / or crystalline atorvastatin particles having a particle size (d ~ 90 ~) of less than 150 µm and an average particle size ( d ~ 50 ~) which is between about 5 and 50 <109> m. Atorvastatin may be one or more of atorvastatin calcium, atorvastatin magnesium, atorvastatin aluminum, atorvastatin iron and atorvastatin zinc. Atorvastatin formulations may be stabilized by mixing atorvastatin with an alkali metal salt additive at a concentration between approximately 1.2% and less than 5% weight / weight of the formulation. The alkali metal salt additive may be one or more of sodium carbonate, sodium bicarbonate, sodium hydroxide, sodium silicate, disodium monohydrate phosphate, sodium dihydrogen phosphate, disodium monohydrate phosphate, sodium phosphate sodium, sodium aluminate, calcium carbonate, calcium hydroxide, magnesium carbonate, magnesium hydroxide, magnesium silicate, magnesium aluminate and magnesium aluminum hydroxide. Atorvastatin formulations may be used to treat medical conditions including primary hypercholesterolaemia, dysbetalipoproteinemia, and familial homozygous hypercholesterolaemia.

BR0307720-9A 2002-02-14 2003-02-14 Alkali Metal Addition Stabilized Atorvastatin Formulations, Method for Producing a Pharmaceutical Formulation and Stabilizing Said Formulation BR0307720A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN112DE2002 2002-02-14
PCT/IB2003/000505 WO2003068191A1 (en) 2002-02-14 2003-02-14 Formulations of atorvastatin stabilized with alkali metal additions

Publications (1)

Publication Number Publication Date
BR0307720A true BR0307720A (en) 2005-01-25

Family

ID=27620520

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0307720-9A BR0307720A (en) 2002-02-14 2003-02-14 Alkali Metal Addition Stabilized Atorvastatin Formulations, Method for Producing a Pharmaceutical Formulation and Stabilizing Said Formulation

Country Status (23)

Country Link
US (1) US20030175338A1 (en)
EP (1) EP1336405A1 (en)
JP (1) JP2005522444A (en)
KR (1) KR20040101229A (en)
CN (1) CN1642526A (en)
AP (1) AP2004003112A0 (en)
AR (1) AR038839A1 (en)
AU (1) AU2003245736A1 (en)
BR (1) BR0307720A (en)
CA (1) CA2475722A1 (en)
CO (1) CO5600997A2 (en)
EA (1) EA200401059A1 (en)
EC (1) ECSP045235A (en)
HR (1) HRP20040829A2 (en)
IL (1) IL163550A0 (en)
IS (1) IS7404A (en)
MX (1) MXPA04007905A (en)
NO (1) NO20043790L (en)
OA (1) OA12777A (en)
PE (1) PE20030935A1 (en)
PL (1) PL371337A1 (en)
WO (1) WO2003068191A1 (en)
ZA (1) ZA200406970B (en)

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Also Published As

Publication number Publication date
EP1336405A1 (en) 2003-08-20
CA2475722A1 (en) 2003-08-21
EA200401059A1 (en) 2005-02-24
US20030175338A1 (en) 2003-09-18
JP2005522444A (en) 2005-07-28
ZA200406970B (en) 2005-06-20
AP2004003112A0 (en) 2004-09-30
PL371337A1 (en) 2005-06-13
OA12777A (en) 2006-07-06
CO5600997A2 (en) 2006-01-31
NO20043790L (en) 2004-11-08
WO2003068191A1 (en) 2003-08-21
AU2003245736A1 (en) 2003-09-04
ECSP045235A (en) 2004-09-28
HRP20040829A2 (en) 2006-07-31
PE20030935A1 (en) 2003-10-30
IL163550A0 (en) 2005-12-18
KR20040101229A (en) 2004-12-02
MXPA04007905A (en) 2004-11-26
AR038839A1 (en) 2005-01-26
IS7404A (en) 2004-08-13
CN1642526A (en) 2005-07-20

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

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